TWI481608B - 作為ｊａｋ抑制劑之咪唑並吡啶衍生物 - Google Patents

作為ｊａｋ抑制劑之咪唑並吡啶衍生物 Download PDF

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Publication number
TWI481608B
TWI481608B TW099144773A TW99144773A TWI481608B TW I481608 B TWI481608 B TW I481608B TW 099144773 A TW099144773 A TW 099144773A TW 99144773 A TW99144773 A TW 99144773A TW I481608 B TWI481608 B TW I481608B
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Taiwan
Prior art keywords
pyridin
group
imidazo
pyrimidin
fluoroimidazo
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TW099144773A
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English (en)
Chinese (zh)
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TW201130835A (en
Inventor
Paul Robert Eastwood
Rodriguez Jacob Gonzalez
Santacana Lluis Miquel Pages
Moll Joan Taltavull
Javaloyes Juan Francisco Caturla
Matassa Victor Giulio
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Almirall Sa
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Application filed by Almirall Sa filed Critical Almirall Sa
Publication of TW201130835A publication Critical patent/TW201130835A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A—HUMAN NECESSITIES
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    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
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    • A61P27/14—Decongestants or antiallergics
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Otolaryngology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Transplantation (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
TW099144773A 2009-12-24 2010-12-20 作為ｊａｋ抑制劑之咪唑並吡啶衍生物 TWI481608B (zh)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09382303A EP2338888A1 (en) 2009-12-24 2009-12-24 Imidazopyridine derivatives as JAK inhibitors

Publications (2)

Publication Number Publication Date
TW201130835A TW201130835A (en) 2011-09-16
TWI481608B true TWI481608B (zh) 2015-04-21

Family

ID=42136251

Family Applications (1)

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TW099144773A TWI481608B (zh) 2009-12-24 2010-12-20 作為ｊａｋ抑制劑之咪唑並吡啶衍生物

Country Status (25)

Country Link
US (1) US20130216498A1 (ko)
EP (2) EP2338888A1 (ko)
JP (1) JP2013515688A (ko)
KR (1) KR20120118459A (ko)
CN (1) CN102695706A (ko)
AR (1) AR079689A1 (ko)
AU (1) AU2010335556A1 (ko)
BR (1) BR112012015540A2 (ko)
CA (1) CA2785113A1 (ko)
CL (1) CL2012001379A1 (ko)
CO (1) CO6541643A2 (ko)
CR (1) CR20120334A (ko)
EA (1) EA201200938A1 (ko)
EC (1) ECSP12011910A (ko)
GT (1) GT201200207A (ko)
IL (1) IL219916A0 (ko)
MX (1) MX2012007175A (ko)
NZ (1) NZ599932A (ko)
PE (1) PE20121482A1 (ko)
SG (2) SG181439A1 (ko)
TW (1) TWI481608B (ko)
UA (1) UA107951C2 (ko)
UY (1) UY33130A (ko)
WO (1) WO2011076419A1 (ko)
ZA (1) ZA201203326B (ko)

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EP2554544A1 (en) 2011-08-01 2013-02-06 Almirall, S.A. Pyridin-2(1h)-one derivatives as jak inhibitors
JP6307096B2 (ja) 2013-01-23 2018-04-04 アストラゼネカ アクチボラグ 化合物
EP3269716B1 (en) * 2013-03-14 2020-09-16 Galapagos N.V. Novel compounds and pharmaceutical compositions thereof for the treatment of inflammatory disorders
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WO2015091531A1 (en) * 2013-12-19 2015-06-25 Almirall, S.A. Imidazolopyrimidin-2-yl derivatives as jak inhibitors
WO2015109285A1 (en) * 2014-01-20 2015-07-23 Cleave Biosciences, Inc. FUSED PYRIMIDINES AS INHIBITORS OF p97 COMPLEX
EP3116506B1 (en) 2014-03-13 2019-04-17 Merck Sharp & Dohme Corp. 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
TWI679205B (zh) 2014-09-02 2019-12-11 日商日本新藥股份有限公司 吡唑并噻唑化合物及醫藥
FR3030521B1 (fr) * 2014-12-23 2019-07-26 Galderma Research & Development Nouveaux composes heterocycliques et leur utilisation en medecine ainsi qu'en cosmetique
EP3250572B1 (en) * 2015-01-28 2020-08-26 Shanghai Fudan-Zhangjiang Bio-Pharmaceutical Co., Ltd. Substituted imidazo [1, 2-a]pyridin-2-ylamine compounds, and pharmaceutical compositions and methods of use thereof
TW201705961A (zh) 2015-06-11 2017-02-16 阿爾米雷爾有限公司 作為ｊａｋ抑制劑的２－（吡唑并吡啶－３－基）嘧啶衍生物
EP3371186A1 (en) 2015-11-03 2018-09-12 Theravance Biopharma R&D IP, LLC Jak kinase inhibitor compounds for treatment of respiratory disease
TWI712604B (zh) 2016-03-01 2020-12-11 日商日本新藥股份有限公司 具jak抑制作用之化合物之結晶
MX2018015483A (es) 2016-06-13 2019-03-18 Glaxosmithkline Ip Dev Ltd Piridinas sustituidas como inhibidores de adn metiltransferasa-1 (dnmt1).
WO2018013430A2 (en) 2016-07-12 2018-01-18 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus infection
AU2018231035B2 (en) * 2017-03-09 2021-09-09 Theravance Biopharma R&D Ip, Llc Fused imidazo-piperidine JAK inhibitors
CA3059785A1 (en) 2017-05-01 2018-11-08 Theravance Biopharma R&D Ip, Llc Methods of treatment using a jak inhibitor compound
CN111867581B (zh) * 2018-01-29 2023-12-26 默克专利股份有限公司 Gcn2抑制剂及其用途
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
EP3892617A4 (en) * 2018-12-07 2022-08-31 Unimatec Co., Ltd. FLUORINATED PYRIMIDINE COMPOUND AND METHOD FOR PRODUCTION THEREOF
US20220143049A1 (en) 2019-03-21 2022-05-12 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
EP4003992A1 (en) 2019-07-24 2022-06-01 Merck Patent GmbH 4-(imidazo[1,2-a]pyridin-3-yl) -pyrimidine derivatives
EP4052759A4 (en) * 2019-11-01 2023-12-20 Unimatec Co., Ltd. FLUORINE-CONTAINING PYRIMIDINE COMPOUND AND METHOD FOR THE PRODUCTION THEREOF
EP4054579A1 (en) 2019-11-08 2022-09-14 Institut National de la Santé et de la Recherche Médicale (INSERM) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
JP7349551B2 (ja) * 2020-02-12 2023-09-22 ユニマテック株式会社 含フッ素ピリミジン化合物およびその製造方法
JP7230274B2 (ja) * 2020-03-25 2023-02-28 ユニマテック株式会社 含フッ素ピリミジン化合物およびその製造方法
AU2022319843A1 (en) * 2021-07-30 2024-03-14 Children's Hospital Medical Center Multi-cyclic irak and flt3 inhibiting compounds and uses thereof
WO2023239941A1 (en) * 2022-06-10 2023-12-14 Interline Therapeutics Inc. Imidazo(1,2-a)pyridine derivatives as ripk2 inhibitors
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